桦木酸及其衍生物的制备与抗肿瘤作用的研究进展

Progress in the Preparation and Anti-Tumor Effect of Betulinic Acid and Its Derivatives

桦木酸是一种羽扇豆烷型的五环三萜类化合物,因具有显著的抗肿瘤和抗HIV病毒特性而受到人们关注。桦木酸存在于多种植物中,可以用提取法得到,但由于桦木酸在植物中含量低,其主要来源是由合成法得到。许多桦木酸衍生物也具有抗肿瘤活性。本文介绍了桦木酸的提取与合成等制备方法,以及几种桦木酸衍生物的合成路线,并对桦木酸及其衍生物的抗肿瘤途径和机理进行了概述。

Betulinic acid as a kind of pentacyclic triterpenoid lupine has caught wide attention due to the significant anti-tumor and anti-HIV viral properties. Betulinic acid existing in many plants can be obtained by extraction method. Because of the low content in plants,betulinic acid is obtained mainly by chemical synthesis. A series of betulinic acid derivatives also have antitumor activity. In this paper,both extraction and chemical synthesis methods of betulinic acid as well as the synthetic routes of betulinic acid derivatives are reviewed. The anti-tumor pathways and mechanisms of betulinic acid and its derivatives are also outlined.